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616451 TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem

The TGF-β RI Kinase Inhibitor, also referenced under CAS 396129-53-6, controls the biological activity of TGF-β RI Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dep

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Synonyms: [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, LY-364947, HTS-466284

Primary Target: TGF-β receptor I kinase
616451
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Overview

Key Spec Table

CAS #Empirical Formula
396129-53-6C₁₇H₁₂N₄

Products

Catalogue NumberPackaging Qty/Pack
616451-5MG Plastic ampoule 5 mg
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Description
OverviewA cell-permeable diheteroaryl-substituted pyrazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β Receptor I kinase (IC50 = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC50 = 740 nM). Shown to inhibit TGF-β-dependent cellular growth (IC50 = 89 nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50 = 47 nM in mink lung cells).
Catalogue Number616451
Brand Family Calbiochem®
Synonyms[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, LY-364947, HTS-466284
References
ReferencesSawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.
Product Information
CAS number396129-53-6
ATP CompetitiveY
FormBrown solid
Hill FormulaC₁₇H₁₂N₄
Chemical formulaC₁₇H₁₂N₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ200
Biological Information
Primary TargetTGF-β receptor I kinase
Primary Target IC<sub>50</sub>51 nM against TGF-β Receptor I kinase; 89 nM against TGF-β-dependent cellular growth in NIH 3T3 mouse fibroblasts; 47 nM against TGF-β-dependent transcription activation in mink lung cells
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Carcinogenic / Teratogenic
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
616451-5MG 04055977185805